Home MAPK ERK inhibitor Ulixertinib (BVD-523)

Ulixertinib (BVD-523)

Catalog No.S7854 Synonyms: VRT752271

For research use only.

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Ulixertinib (BVD-523) Chemical Structure

CAS No. 869886-67-9

Selleck's Ulixertinib (BVD-523) has been cited by 39 publications

Purity & Quality Control

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Biological Activity

Description Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Targets
ERK1 [1] ERK2 [1]
<0.3 nM
In vitro

In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 NYL6UHl{TnWwY4Tpc44h[XO|YYm= M1vCR2lvcGmkaYTpc44hd2ZiRWLLNkBqdiCqdX3hckBCOzd3IHPlcIx{KGijcnLvdolv\yCEUlHGJHY3ODCHIH31eIFvfCCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBxcG:|cHjvdplt[XSnZDDSV2shdGW4ZXzzMEBKSzVyIE2gNE4xOzFizszNMi=> NVmwdZoxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizO|Y{ODZpPkK4N|c3OzB4PD;hQi=>
A375 NF;Xd2pHfW6ldHnvckBie3OjeR?= NWDvXmJFOiCqcoO= NYnFcpg{UW6qaXLpeIlwdiCxZjDFVmsyNzJiaX6gbJVu[W5iQUO3OUBk\WyuczDoZZJjd3KrbnegRk1TSUZiVk[wNGUhdXW2YX70JIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIIDoc5NxcG9vUmPLJIxmfmWuIHHmeIVzKDJiaILzJIJ6KEOnbHzvcYlkeyCDcoLhfXNk[W6WTTDWWGkhcW2jZ3nu[{BidmGueYPpd{whUUN3MDC9JFAvOTRizszNMi=> Mn3LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7N{e5PFEoRjJ3OUe3PVgyRC:jPh?=
A375 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NUe1XGh5PzJiaILz M{XXfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDoZZJjd3KrbnegRk1TSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[Yxtd22rY4OgRZJz[XmVY3HuWG0hXlSLIHntZYdqdmdiYX7hcJl{cXNuIFnDOVAhRSByLkG4JO69VS5? M2[1V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe3PVgyLz5{NUm3O|k5OTxxYU6=
SKCO1 NF7FV5dCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4\FZ|czKGi{cx?= NYDITWpzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2NQOSClZXzsd{Bp[XKkb4LpcochU1KDUzDHNVJXKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFAvOzV4IN88UU4> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB|OEm0NEc,OjhyM{i5OFA9N2F-
BA/F3 MVvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M3vzVlczKGi{cx?= NIrZS5ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIhiemKxcnnu[{BMWkGVIFexNmQhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNE41PjhizszNMi=> MmPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{i5OFAoRjJ6MEO4PVQxRC:jPh?=
SW620 Ml3DRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MlniO|IhcHK| M4TjU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgbIFz[m:{aX7nJGtTSVNiR{GyWkBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCwMlQ6QSEQvF2u MnywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{i5OFAoRjJ6MEO4PVQxRC:jPh?=
AsPC1 M{Ly[2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYXhbnVkPzJiaILz M3S2NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQYPQR|Eh[2WubIOgbIFz[m:{aX7nJGtTSVNiR{GySEBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCwMlg1QSEQvF2u MlzuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{i5OFAoRjJ6MEO4PVQxRC:jPh?=
NCI-H23 NInRXVRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVqwfm1xPzJiaILz MlG4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFI{KGOnbHzzJIhiemKxcnnu[{BMWkGVIFexNmMhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNUDPxE1w NHP1OZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECzPFk1OCd-MkiwN|g6PDB:L3G+
SW156 NHviS|RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVq3NkBpenN? M3;UfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2exOVYh[2WubIOgbIFz[m:{aX7nJJdqdGRidInw[UBMWkGVIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMT6yOEDPxE1w NVvBeXpURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwN|g6PDBpPkK4NFM5QTRyPD;hQi=>
BA/F3 NUDve4toSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NFjTeXM4OiCqcoO= NInjOJZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNk4zOzFizszNMi=> M3nuTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4PVQxLz5{OECzPFk1ODxxYU6=
A375 MUXGeY5kfGmxbjDhd5NigQ>? MWeyJIhzew>? M2fqPWlvcGmkaYTpc44hd2ZiRWLLNkBqdiCqdX3hckBCOzd3IHPlcIx{KGijcnLvdolv\yCELWLBSkBXPjByRTDteZRidnRiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4heGixc4Doc{1GWkt{IHzleoVtKGGodHXyJFIhcHK|IHL5JGNmdGyxbXnjd{BCenKjeWPjZY5VVSCYVFmgbY1i\2mwZzDhcoFtgXOrczygTWM2OCB;IESuNUDPxE1w NVTkVVI5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5O|c6QDFpPkK1PVc4QThzPD;hQi=>
A375 MlXmSpVv[3Srb36gZZN{[Xl? NGrzTmhKdmirYnn0bY9vKG:oIFXST|IhcW5iaIXtZY4hSTN5NTDj[YxteyCqYYLic5JqdmdiQmLBSkBXPjByRTDteZRidnRiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4heGixc4Doc5J6dGG2ZXSgSXJMOiCuZY\lcJMtKEmFNUCgQUA1NjFizszNMi=> M4XGeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|A3Lz5{OEO3OlMxPjxxYU6=
BA/F3 NG\ScZVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2rvN|czKGi{cx?= NIG1Nm5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIhiemKxcnnu[{BMWkGVIFexNmQhdXW2YX70JIFnfGW{IEeyJIhzeyCrbjDwdoV{\W6lZTDv[kBKVC1|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUCgQUA5NjZyODFOwG0v MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB|OEm0NEc,OjhyM{i5OFA9N2F-
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-ERK / ERK / RRM2 28797284
Growth inhibition assay Cell viability 30771617

Protocol (from reference)

Kinase Assay:[1]
  • ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:

    MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
Cell Research:[1]
  • Cell lines: A375 cells
  • Concentrations: ~30 μM
  • Incubation Time: 72 h
  • Method: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.

Solubility (25°C)

In vitro

 DMSO 86 mg/mL
(198.46 mM)
Ethanol 15 mg/mL
(34.61 mM)
Water Insoluble

Chemical Information

Molecular Weight 433.33
Formula

C21H22Cl2N4O2
CAS No. 869886-67-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04488003 Recruiting Drug: Ulixertinib|Drug: Physician''s Choice Advanced Solid Tumor|BRAF Gene Mutation|BRAF Gene Alteration|MEK Mutation|MEK Alteration|MAP2K1 Gene Mutation|MAP2K1 Gene Alteration|MAP2K2 Gene Mutation|MAP2K2 Gene Alteration BioMed Valley Discoveries Inc November 3 2020 Phase 2
NCT04145297 Recruiting Drug: Ulixertinib|Drug: Hydroxychloroquine Gastrointestinal Neoplasms University of Utah|BioMed Valley Discoveries Inc March 17 2020 Phase 1
NCT03698994 Active not recruiting Other: Pharmacokinetic Study|Drug: Ulixertinib Advanced Malignant Solid Neoplasm|Recurrent Ependymal Tumor|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Primary Malignant Central Nervous System Neoplasm|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Primary Malignant Central Nervous System Neoplasm|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Wilms Tumor National Cancer Institute (NCI) October 1 2018 Phase 2
NCT03417739 Active not recruiting Drug: BVD-523 Uveal Melanoma Dana-Farber Cancer Institute|BioMed Valley Discoveries Inc March 26 2018 Phase 2
NCT02994732 Completed Drug: [14C]-BVD-523 Healthy BioMed Valley Discoveries Inc January 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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